1. Anti-infection Metabolic Enzyme/Protease MAPK/ERK Pathway GPCR/G Protein
  2. HCV HCV Protease Ras
  3. BI-1388

BI-1388 is a macrocyclic acylsulfonamide-based HCV NS3-4A protease inhibitor. BI-1388 inhibits clinically relevant drug-resistant mutant strains (KRASD168V gt 1b and KRASR155K gt 1a) and exhibits high liver distribution. BI-1388 is applicable for the research of HCV infection.

For research use only. We do not sell to patients.

The BI-1388 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

BI-1388

BI-1388 Chemical Structure

CAS No. : 1309952-03-1

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Description

BI-1388 is a macrocyclic acylsulfonamide-based HCV NS3-4A protease inhibitor. BI-1388 inhibits clinically relevant drug-resistant mutant strains (KRASD168V gt 1b and KRASR155K gt 1a) and exhibits high liver distribution. BI-1388 is applicable for the research of HCV infection[1].

IC50 & Target[1]

K-RAS

 

In Vitro

BI-1388 (compound 19) inhibits the replication of HCV genotype 1b D168V variant, with an EC50 of 1.0 nM at 72 h; it also inhibits the replication of HCV genotype 1a R155K variant, with an EC50 of 0.14 nM at 72 h[1].
The half-life of BI-1388 in human liver microsomes is 54 min[1].
The half-life of BI-1388 in rat liver microsomes is 138 min[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route Cmax AUC T1/2 Vss CL Bioavailability
Rat[1] 10 mg/kg p.o. 1.3 μM 1.4 μM·h / / / /
Rat[1] 4 mg/kg i.v. / / 2.6 h 0.97 L/kg 19 mL/min/kg 14 %
Molecular Weight

819.97

Formula

C41H53N7O9S

CAS No.
SMILES

O=C([C@]([C@]1([H])/C=C\CCCCC[C@@H]2NC(C3=NN(C)C=C3)=O)(C1)NC([C@@](C[C@@H](OC4=CC(OC(C)C)=NC5=C(C)C(OC)=CC=C45)C6)([H])N6C2=O)=O)NS(=O)(C7(C)CC7)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BI-1388
Cat. No.:
HY-115516
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